Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0043352 (xerostomia)
 4,250 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Pharmacokinetics of 3 doses (70 mg, 105 mg and 140 mg) of lofepramine were compared with amitriptyline (50 mg) in 6 healthy drug free elderly subjects aged between 65 and 72 years. Pharmacokinetics of lofepramine in the elderly appear to be similar to young adults as published before. Peak plasma lofepramine and amitriptyline concentrations were achieved at about 1 h and 3 h of dosing respectively. Elimination half-life of lofepramine was 2.5 h and that of amitriptyline was 31 h. A 24-fold inter-individual variation in peak plasma lofepramine concentrations was observed, but amitriptyline levels in plasma showed less variation. Pharmacokinetic parameters of amitriptyline were comparable to other published studies involving elderly people. Compared to placebo and lofepramine, amitriptyline produced drowsiness and dry mouth, reduced salivary volume and increased movement reaction time. These effects correlated with the plasma amitriptyline levels.
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PMID:Pharmacokinetics of lofepramine and amitriptyline in elderly healthy subjects. 267 25

The clinical records of 25 ambulatory patients who received clonidine (Catapres-TTS) for periods of one to 19 months were reviewed to determine the effectiveness and long-term patient tolerance of this transdermal antihypertensive medication. In 11 patients with mild to moderate hypertension in whom Catapres-TTS was initiated as monotherapy or added to an oral diuretic, significant blood pressure reduction was observed during the initial four weeks of therapy. In 14 patients who had more severe hypertension and who were receiving multiple antihypertensive agents, Catapres-TTS did not result in significantly reduced blood pressure. Daily home blood pressure measurements in five patients showed no day-to-day variations in blood pressure during the seven days each patch was worn. Catapres-TTS was discontinued in 11 patients because of localized contact dermatitis (six patients), patient dissatisfaction (three patients), and physician's decision (two patients). In three patients, localized contact dermatitis developed only after continuous use for periods of four to 13 months. Other adverse effects such as drowsiness and dry mouth were less apparent than with comparable doses of oral clonidine, and did not necessitate discontinuation of therapy in any patient. Black patients appear to tolerate Catapres-TTS better than whites. Catapres-TTS appears to be effective in patients with mild to moderate hypertension and may be a useful alternative to oral clonidine in patients experiencing drowsiness or dry mouth with the oral preparation.
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PMID:Patient acceptance of transdermal clonidine. A retrospective review of 25 patients. 273 24

Seventy-six consecutive patients receiving chemotherapy were evaluated for the antiemetic efficacy and side-effects of the combination of chlorpromazine (CPM) and methylprednisolone (MPN). All patients had previously received the same chemotherapy with metoclopramide in conventional dosage and experienced severe emesis. A significant antiemetic response was achieved in 70% of the patients, and in 28% of them the antiemetic protection was complete. The most common side effects were drowsiness, dry mouth and headache. The combination of CPM and MPN is effective, well tolerated and is recommended for outpatients receiving chemotherapy for cancer.
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PMID:Methylprednisolone and chlorpromazine in patients receiving cancer chemotherapy: a prospective non-randomized study. 273 82

Long-term antihypertensive treatment by once-weekly application of transdermal clonidine patches, in doses equivalent to 0.1, 0.2, 0.3 mg of clonidine daily, was evaluated in an open trial of 41 patients with baseline seated diastolic blood pressures of 90 to 103 mmHg. In all the patients, seated diastolic blood pressure was reduced to less than 90 mmHg with transdermal clonidine alone at the end of a dose titration phase of two to six weeks. Thirty-two patients successfully completed at least 22 months of therapy; three patients withdrew because of lack of efficacy and six because of adverse events. In the second treatment year 14 patients required a concomitant diuretic. Mean reductions in seated diastolic blood pressure from baseline values were statistically significant (P less than 0.0001) at all study intervals. The incidence of patient withdrawals resulting from the development of contact dermatitis at the patch application site was 5%; skin irritation not requiring withdrawal occurred in 13 patients during the first year of treatment and in two during the second. The incidence of dry mouth (in 7%) and drowsiness (in 10%) was lower than has been reported during oral clonidine therapy (40% and 35%). The results suggest that transdermal clonidine may be beneficial for the maintenance therapy of many patients with mild hypertension.
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PMID:Long-term treatment with transdermal clonidine in mild hypertension. 274 74

Acceptability and plasma concentrations of rilmenidine, a new antihypertensive agent mainly eliminated via the kidney, were evaluated in 17 hypertensive patients (supine diastolic blood pressure, 104 +/- 3 mmHg) with renal insufficiency (creatinine clearance, 35 +/- 4 ml.minute-1/1.73 m2; range, 12 to 58). Patients were treated for six months with rilmenidine at the dose of 1 mg in the morning or 1 mg twice daily as single-drug therapy in untreated patients, or in combination or as substitution in patients already treated. Plasma concentrations of rilmenidine were measured by gas chromatography combined with mass spectrometry at Days 0, 1, 5, 7, 9, and 11, and Months 1.5, 3, 4.5, and 6 before administration. Supine and erect blood pressure (sphygmomanometer) measurements and side effects were noted at the same times. Laboratory and electrocardiographic parameters were evaluated at Days 0 and 11, and Months 1.5 and 6. Blood pressure was effectively controlled during the trial in 12 patients (mean decrease in systolic/diastolic blood pressure of 12/8 mmHg). Five patients were removed from the trial after Month 1.5 because of a rise in blood pressure (three cases) or noncompliance (two cases). Side effects were moderate and transient (dry mouth, constipation, daytime drowsiness, mood disturbances, insomnia) never requiring treatment withdrawal. Surveillance of renal function revealed no significant mean variation. Rilmenidine plasma concentrations reached steady state the fifth day at the latest and were related to the degree of renal insufficiency. When renal function was stable (13 cases), plasma concentrations did not vary until the end of the trial. When renal function was progressive (four cases), plasma concentrations increased in parallel in two patients, without the onset of side effects, and remained stable in the other two patients. In conclusion, this study confirmed the good acceptability of rilmenidine in hypertensive patients with chronic renal insufficiency. It showed stable plasma concentrations of rilmenidine during a six-month treatment in hypertensive patients with renal insufficiency, reflecting the absence of accumulation of the drug.
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PMID:Acceptability of rilmenidine and long-term surveillance of plasma concentrations in hypertensive patients with renal insufficiency. 278 26

Much of our knowledge about the CNS control of blood pressure is derived from animal studies using techniques such as intracerebroventricular administration of drugs, stereotactic ablation of specific brain nuclei, and biochemical analysis of these nuclei. These methods have identified numerous specific brain nuclei in the brain stem and a meshwork of interconnecting neurones involved in cardiovascular control. The main neurotransmitter involved is noradrenaline but recent interest has focused on several laterally situated nuclei which are capable of synthesizing adrenaline. Centrally acting antihypertensive drugs are thought to act by stimulating central alpha 2-adrenoceptors either by the parent drug itself (clonidine) or via the formation of an active metabolite (alpha-methyldopa). This leads to decreased peripheral sympathetic activity and a hypotensive response but the latter is often attained at the expense of central side-effects such as drowsiness or dry mouth. The mechanism of the antihypertensive effect of beta-blockers remains uncertain although the balance of evidence is against a central effect. The central administration of propranolol causes decreased peripheral sympathetic activity in animals, but plasma catecholamine levels are little altered by beta-blockers in man. In equipotent antihypertensive doses, central alpha-agonists cause a much greater reduction in plasma noradrenaline than beta-blockers.
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PMID:Central nervous system mechanisms in blood pressure control. 286 46

Thirteen healthy subjects participated in a combined acute and subacute double-blind, cross-over trial of two H1-antihistamines diphenhydramine (DPH) and temelastine (SKF) against placebo. The doses were DPH 50 mg b.d. and SKF 100 mg b.d. Objective (digit symbol substitution, flicker fusion, Maddox wing, attention, tracking, choice reaction) and subjective (visual analogue scales, side-effects on questionnaire) tests were done on Days 1, 4 and 5, on each occasion before drug intake and after 90 min and 3 h. On Day 1 DPH caused clear sedation of unpleasant character and impaired flicker fusion, attention and digit symbol substitution. SKF shifted the VAS assessment "drowsy/alert" towards drowsiness at 90 min, without objective impairment. On Day 4 DPH reduced exophoria and impaired flicker fusion without subjective sedation. On Day 5, diazepam 0.3 mg/kg (DZ) given with the other drugs caused subjective sedation of pleasant character and impaired various functions in the objective tests. Neither SKF nor DPH increased the effects of DZ; DPH slightly counteracted the effect of DZ on exophoria. At home, SKF did not differ from placebo while DPH proved sedative. DPH did not improve sleep but caused dry mouth and blurred vision. Measurement of plasma levels of antihistamines on each test day revealed the development of tolerance to antihistamine-induced sedation. The concentration of DZ measured by bioassay was somewhat elevated in the presence of DPH. Since the majority of the performance tests were not influenced by temelastine, it appears to be an acceptable, novel H1-antihistamine for the treatment of allergic disorders.
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PMID:Acute and subacute actions on human performance and interactions with diazepam of temelastine (SK&F93944) and diphenhydramine. 287 12

Astemizole, a new histamine H1 receptor antagonist, was tested in a double-blind cross-over comparison study with chlorpheniramine maleate, a very effective conventional H1 antagonist, in patients with chronic allergic rhinitis. Astemizole was found to be equally effective, yet there was a significant decrease in the side effects of sleepiness (P less than .01) and dry mouth (P less than .05). Astemizole has a completely different structure and binding curves from terfenadine. It is approved for clinical use in the United Kingdom, Canada, and many European countries.
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PMID:Efficacy of an H1 antagonist, astemizole, for chronic allergic rhinitis. 288 23

A double-blind multicenter trial compared rilmenidine with placebo in the treatment of 126 patients with mild to moderate hypertension after a 4-week placebo run-in period. Patients with mild hypertension (study 1) with mean supine diastolic blood pressure (BP) between 95 and 104 mm Hg received either rilmenidine 1 mg/day (n = 31) or placebo (n = 35) for 4 weeks. In study 2, patients with moderate hypertension (mean supine diastolic BP between 105 and 115 mm Hg) received either rilmenidine 1 mg twice a day (n = 30) or placebo twice a day (n = 30) for 4 weeks. All 61 patients taking rilmenidine completed the study; 8 of the 65 patients taking placebo were withdrawn because of an increase in BP. Rilmenidine significantly reduced mean systolic and diastolic BP compared with placebo in both studies. BP was normalized (systolic less than 160 mm Hg and diastolic less than or equal to 90 mm Hg in 61% of the patients taking rilmenidine as opposed to 23% of those taking placebo (p less than 0.001). There was no significant difference in the incidence of either dry mouth or daytime drowsiness between rilmenidine, 1 mg/day, and placebo. Dry mouth was significantly more frequent with rilmenidine, 2 mg/day, than with placebo, but this difference was transient and no longer significant at the end of the study. No unexpected adverse effects occurred. Rilmenidine as single therapy appears to be effective and well accepted in the management of mild to moderate hypertension, in particular at the 1-mg/day dose, which normalized 84% of mild hypertensive patients and did not induce any significant adverse effects compared with placebo.
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PMID:Efficacy and acceptability of rilmenidine for mild to moderate systemic hypertension. 289 64

To assess the long-term acceptability and efficacy of rilmenidine (S 3341), patients with placebo-resistant hypertension (diastolic blood pressure [BP] greater than or equal to 95 mm Hg and less than 115 mm Hg) were included in an open 1-year treatment study. Eight examinations allowed treatment adaptation if diastolic BP remained greater than or equal to 90 mm Hg (monotherapy with rilmenidine, 1 or 2 mg/day, followed by the addition of a diuretic, then tritherapy). Three hundred seventeen patients, aged 58.0 +/- 0.7 years, were included. Two hundred sixty-nine were followed for 1 year and 48 withdrew from the trial without any symptom suggesting a withdrawal syndrome: 4 because of adverse effects; 6, lack of efficacy despite triple therapy; 9, intercurrent diseases; 10, noncompliance independent of adverse effects; 18, personal reasons not associated with treatment; and 1, lost to follow-up. On the 12th month, the decrease in supine systolic and diastolic BP reached 25 and 17 mm Hg with monotherapy (n = 150), 26 and 17 mm Hg with double therapy (n = 90) and 20 and 15 mm Hg with triple therapy (n = 29). BP was normalized (diastolic BP less than or equal to 90 mm Hg) on months 6 and 12 in 80 and 84% of the patients, respectively. Monotherapy was maintained in 66 and 60% of these patients, respectively, two-thirds being treated with 1 mg once daily. Adverse effects with monotherapy were mainly observed at the beginning of treatment in 3 to 8%: dry mouth, asthenia, gastralgia, palpitations, drowsiness, insomnia; other adverse effects were rare (1 to 2%).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Efficacy and safety of rilmenidine for arterial hypertension. 289 68


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